This invention relates to substituted biguanides suitable for diabetes mellitus therapy.
Three compounds of the class of substituted biguanides are utilized for the treatment of diabetes mellitus, viz., 1-butylbiguanide, 1-.beta.-phenethylbiguanide (phenformin), and 1,1-dimethylbiguanide (metformin). A characteristic of these three compounds is their narrow therapeutic spectrum and their gastrointestinal incompatibility.
It has now been found that the novel 1,2-substituted biguanides of the invention possess as good or better blood-sugar-lowering effect than the above-mentioned commercial products, and a better therapeutic index. For example, the LD.sub.50 in mice of 1-butylbiguanide is 346 mg./kg., whereas the novel 1,2-biguanides can be tolerated without damage in doses of about 2 g./kg.